Merck + Co., Inc.

Stephen E DeLaszlo

William K Hagmann

Theodore M Kamenecka

Malcolm MacCoss

George A Doherty

Linda L Chang

Robert G Johnson

Tsuneo Fujita

Ginger X Yang

Christopher F Reilly

Compounds of Formula I are antagonists of VLA-4 and/or &agr; &bgr; , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Substituted amidine derivatives as inhibitors of cell adhesion

Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Heterocycle amides as cell adhesion inhibitors

Substituted ureas as cell adhesion inhibitors

para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;,&bgr;,, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Para-aminomethylaryl carboxamide derivatives

Azapeptide acids of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Azapeptide acids as cell adhesion inhibitors

4-Substituted-4-piperidinecarboxamides of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

4-substituted-4-piperidine carboxamide derivatives

Novel disubstituted 6-aminoquinazolinones of the Formula ##STR1## are useful as angiotensin-II receptor (subtype 2) antagonists (AT.sub.2 antagonists) alone or in combination with heparin, and can act to suppress the vascular stenosis which commonly occurs during the development of atherosclerosis and the restenosis following arterial angioplasty, stent placement, bypass surgery, heart transplantation or endarterectomy.

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Rumson, NJ, United States of America

Stephen E DeLaszlo